Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

PIP4K2A (P48426) - Overview - Molecular Target Synopsis

Protein


PIP4K2A, Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha
Enzyme Classification 2.7.1.149
UniProt P48426

Also Known as PI42A_HUMAN, PIP4K2A, PIP5K2, PIP5K2A

Catalyzes the phosphorylation of phosphatidylinositol 5-phosphate (PtdIns5P) on the fourth hydroxyl of the myo-inositol ring, to form phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P2). May exert its function by regulating the levels of PtdIns5P, which functions in the cytosol by increasing AKT activity and in the nucleus signals through ING2. May regulate the pool of cytosolic PtdIns5P in response to the activation of tyrosine phosphorylation. May negatively regulate insulin-stimulated glucose uptake by lowering the levels of PtdIns5P. May be involved in thrombopoiesis, and the terminal maturation of megakaryocytes and regulation of their size. Homodimer (By similarity). Interacts with PIP4K2B. Interaction with PIP4K2B may regulate localization to the nucleus.

2YBX
CRYSTAL STRUCTURE OF HUMAN PHOSPHATIDYLINOSITOL-5-PHOSPHATE 4-KINASE TYPE-2 ALPHA
RCSB/PDB
Inspect Structure
See all 3D Structures for PIP4K2A

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PIP4K2A is active in the following subcellular-locations: cell membrane, cytoplasm, nucleus.
GO terms: PIP4K2A is active in the following subcellular-locations: autophagosome, cytosol, nucleoplasm, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PIP4K2A has gain in 5 cell-lines, loss in 8 cell-lines and no signal in 992 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: RXF_393, SK_MEL_5, SK_MEL_2

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H28, SK23, EB1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, HSMM, MCF-7

(see details)

RNA Interference


PIP4K2A was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: H2342, HCC202. (see details)

3D Structures


For PIP4K2A there are:
1 structures (2 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PIP4K2A has been screened with 216 compounds (219 bioactivities), 1 compounds have bioactivities that show binding affinity of <= 500nM (1 bioactivities). (see details)